(1H-Pyrrolo [2,3-b]pyridine)7-Azaindole Derivatives and Their Antiurease, Phosphodiesterase and β-glucuronidase Activity

Abstract

A variety of 7-azaindole analogs 1-14 with variable substituents on phenyl ring of phenacyl moiety were synthesized and evaluate for their urease, phosphodiesterase and b-glucuronidase Inhibitory potential. Compound 9 (IC50 = 2.19±0.37µM) showed potent urease inhibitory potential than standard thiourea (IC50 = 21.00±0.01µM). However, while compounds 10 (IC50 = 255.11±6.62µM) and 8 (IC50 = 133.3±0.46µM), exhibited moderate urease potential. Moreover, compound 2 (IC50 = 20.83± 0.234µM) showed potent phosphodiesterase inhibitory potential than standard EDTA (IC50 = 274.00+0.007µM). Compound 8 (IC50 192.6±3.53µM) was found to be moderate b-glucuronidase inhibitor, as compare to standard 1,4, lactone D saccharic acid (IC50 = 48.41±1.24µM). Nevertheless, compounds 13 (36.81% inhibition) and 14 (47.11% inhibition) showed less than 50% b-glucuronidase inhibition, therefore they were not further evaluated for their IC50 values. The size of the substituent, electron donating or withdrawing affect of substituents as well as the position of substituent on phenyl affects the activity.